BAM7

製品コードS7105 バッチS710501

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H19N5O2S
分子量 405.47 CAS No. 331244-89-4
Solubility (25°C)* 体外 DMSO 2 mg/mL warmed with 50ºC water bath (4.93 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.
in vitro BAM7 directly binds the previously uncharacterized BH3-binding groove at the N-terminal face of BAX. BAM7 is selective for the BH3-binding groove at the N-terminal face of BAX. BAM7 directly interacts with BAX at the very surface used by the BIM BH3 helix to trigger BAX activation. BAM7 results in functional BAX activation. BAM7 triggers the conversion of BAX from monomer to oligomer in a dose- and time-responsive manner, the kinetics of which approach saturation at a 1:8 dose ratio of BAX:BAM7. BAM7 triggers in vitro BAX oligomerization, BAX-mediated pore formation and BAX-dependent cell death. BAM7 selectively induces BAX-mediated apoptosis by triggering the hallmark features of intracellular BAX activation. BAM7 only kills the cell line that contains BAX, eliciting the biochemical and morphologic features of BAX-mediated apoptosis. [1]
特徴 Does not interact with the BH3-binding pocket of antiapoptotic proteins or proapoptotic BAK and induces cell death in a BAX-dependent fashion.

プロトコル(参考用のみ)

キナーゼアッセイ Fluorescence polarization binding assays
Direct binding curves are first generated by incubating FITC-BIM SAHB (50 nM) with serial dilutions of fulllength BAX, BCL-XLΔC, MCL-1ΔNΔC, BFL-1/A1ΔC or BAKΔC and fluorescence polarization measured at 20 minutes on a SpectraMax M5 microplate reader. For competition assays, a serial dilution of small molecule or acetylated BIM SAHB (Ac-BIM SAHB) is combined with FITC-BIM SAHB (50 nM), followed by the addition of recombinant protein at ~EC75 concentration, as determined by the direct binding assay (BAX, BAKΔC: 500 nM; BCL-XLΔC, MCL-1ΔNΔC, BFL-1/A1ΔC: 200 nM). Fluorescence polarization is measured at 20 minutes and IC50 values calculated by nonlinear regression analysis of competitive binding curves using Prism software.
細胞アッセイ 細胞株 MEFs
濃度 ~15 μM
反応時間 24 h
実験の流れ MEFs (2.5 × 103 cells per well) are seeded in 96-well opaque plates for 18-24 h and then incubated with serial dilutions of BAM7, ANA-BAM16 or vehicle (0.15% (v/v) DMSO) in DMEM at 37 °C in a final volume of 100 μL. Cell viability is assayed at 24 h by addition of CellTiter-Glo reagent according to the manufacturer’s protocol, and luminescence is measured using a SpectraMax M5 microplate reader. Viability assays are performed in at least triplicate, and the data are normalized to vehicle-treated control wells.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Small-molecule allosteric inhibitors of BAX. [ Nat Chem Biol, 2019, 15(4):322-330] PubMed: 30718816
Survival of midbrain dopamine neurons depends on the Bcl2 factor Mcl1 [ Cell Death Discov, 2018, 4:107] PubMed: 30479840

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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